2022
DOI: 10.1021/acs.jmedchem.2c01271
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Development of MAO-A and 5-HT2AR Dual Inhibitors with Improved Antidepressant Activity

Abstract: Designing dual-target inhibitors targeting 5-HT2AR and MAO-A could synergistically promote interstitial 5-HT levels, so as to exhibit a more efficient antidepressant effect. On the premise of maintaining the original pharmacophore binding, arylpiperazine scaffolds and 5-oxygen-substituted oxoisoaporphines were hybridized to afford 15 dual-target inhibitors through suitable linkers. Among all inhibitors, I 14 exhibited the best inhibitory activities against 5-HT2AR and MAO-A. In vitro cell proliferation assay… Show more

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Cited by 4 publications
(2 citation statements)
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“…Depression is a prevalent and severe mental health challenge that impacts millions of people globally. It ranks third in global disability, and the WHO expects it to be the top cause by 2030. The most widely used therapies for depression are based on the monoamine neurotransmitter hypothesis, which assumes that a deficiency of serotonin or norepin­ephrine in the brain leads to the development of depression. Traditional antidepressants can help some patients overcome depression. However, these drugs have a delayed onset of action, despite quickly altering mono­aminergic transmission.…”
Section: Introductionmentioning
confidence: 99%
See 1 more Smart Citation
“…Depression is a prevalent and severe mental health challenge that impacts millions of people globally. It ranks third in global disability, and the WHO expects it to be the top cause by 2030. The most widely used therapies for depression are based on the monoamine neurotransmitter hypothesis, which assumes that a deficiency of serotonin or norepin­ephrine in the brain leads to the development of depression. Traditional antidepressants can help some patients overcome depression. However, these drugs have a delayed onset of action, despite quickly altering mono­aminergic transmission.…”
Section: Introductionmentioning
confidence: 99%
“…1 H NMR (400 MHz, chloroform-d) δ 7.75 (d, J = 8 3. Hz, 2H), 7.45−7.30 (m, 7H), 4.71 (dd, J = 27.7, 11.2 Hz, 1H), 4.37 (dd, J = 15.9, 11.2 Hz, 1H), 3.79 (s, 3H), 2.45 (s, 3H).…”
mentioning
confidence: 99%